The accelerated preparation of 1,4-dihydropyridines using microflow reactors

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• 作者：Patricia Tambarussi Baraldi^a ; ^b ; Timothy Noë ; l^a ; ^c ; Qi Wang^a ; Volker Hessel^a ; ^{v.hessel@tue.nl" class="auth_mail}
• 关键词：Dihydropyridines ; Multicomponent reaction ; Flow chemistry ; Hantzsch reaction ; Microreactor
• 刊名：Tetrahedron Letters
• 出版年：26 March, 2014
• 年：2014
• 卷：55
• 期：13
• 页码：2090-2092
• 全文大小：586 K

文摘

The synthesis of 1,4-dihydropyridines was performed in a continuous-flow microreactor. Elevated temperatures accelerated the reaction rate significantly allowing the reaction to be finished in minutes (6-11 min). Different 1,4-dihydropyridines were prepared in good to excellent isolated yields (45-88% yield). The method was amenable to the preparation of daropidine, a calcium channel blocker which is currently in clinical phase 3 trials.